scholarly journals Ceftriaxone Absorption Enhancement for Noninvasive Administration as an Alternative to Injectable Solutions

2018 ◽  
Vol 62 (12) ◽  
Author(s):  
Boubakar Ba ◽  
Karen Gaudin ◽  
Amélie Désiré ◽  
Thida Phoeung ◽  
Marie-Hélène Langlois ◽  
...  
Keyword(s):  
Neonatal Sepsis ◽  
Human Subjects ◽  
Rabbit Model ◽  
Absorption Enhancement ◽  
Rectal Absorption ◽  
Noninvasive Treatment ◽  
Absorption Enhancers ◽  
Treatment Delays ◽  
Resource Limited ◽  
Maximal Plasma

ABSTRACT Neonatal sepsis is a major cause of infant mortality in developing countries because of delayed injectable treatment, making it urgent to develop noninjectable formulations that can reduce treatment delays in resource-limited settings. Ceftriaxone, available only for injection, needs absorption enhancers to achieve adequate bioavailability via nonparenteral administration. This article presents all available data on the nonparenteral absorption of ceftriaxone in humans and animals, including unpublished work carried out by F. Hoffmann-La Roche (Roche) in the 1980s and new data from preclinical studies with rabbits, and discusses the importance of these data for the development of noninjectable formulations for noninvasive treatment. The combined results indicate that the rectal absorption of ceftriaxone is feasible and likely to lead to a bioavailable formulation that can reduce treatment delays in neonatal sepsis. A bile salt, chenodeoxycholate sodium salt (Na-CDC), used as an absorption enhancer at a 125-mg dose, together with a 500-mg dose of ceftriaxone provided 24% rectal absorption of ceftriaxone and a maximal plasma concentration of 21 µg/ml with good tolerance in human subjects. The rabbit model developed can also be used to screen for the bioavailability of other formulations before assessment in humans.

Rectal absorption enhancement of insulin in rabbits from hollow-type suppositories by glyceryl-1-monooctanoate

1990 ◽  
Vol 13 (2-3) ◽  
pp. 316-317 ◽  
Author(s):  
Y. Watanabe ◽  
Y. Matsumoto ◽  
N. Hori ◽  
M. Matsumoto
Keyword(s):  
Absorption Enhancement ◽  
Rectal Absorption

The necessity of full sepsis screen in neonatal sepsis: Experience in a resource-limited setting

2016 ◽  
Vol 19 (2) ◽  
pp. 89 ◽  
Author(s):  
KennethIkenna Onyedibe ◽  
MarkOjogba Okolo ◽  
Bose Toma ◽  
Tolulope Afolaranmi
Keyword(s):  
Neonatal Sepsis ◽  
Resource Limited Setting ◽  
Resource Limited ◽  
Sepsis Screen ◽  
Limited Setting

scholarly journals Impact of Sodium N-[8-(2-Hydroxybenzoyl)amino]-caprylate on Intestinal Permeability for Notoginsenoside R1 and Salvianolic Acids in Caco-2 Cells Transport and Rat Pharmacokinetics

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2990 ◽  
Author(s):  
Ying Li ◽  
Dandan Yang ◽  
Chunyan Zhu
Keyword(s):  
Membrane Permeability ◽  
Cell Monolayer ◽  
Salvianolic Acid B ◽  
Absorption Enhancement ◽  
Enhancement Effect ◽  
Absorption Enhancers ◽  
Salvianolic Acid ◽  
Salvianolic Acids

For drugs with high hydrophilicity and poor membrane permeability, absorption enhancers can promote membrane permeability and improve oral bioavailability. Sodium N-[8-(2-hydroxybenzoyl)amino]caprylate (SNAC) is a new kind of absorption enhancer that has good safety. To investigate the absorption enhancement effect of SNAC on non-polar charged and polar charged drugs and establish the absorption enhancement mechanism of SNAC, SNAC was synthesized and characterized. Two representative hydrophilic drugs—notoginsenoside R1 (R1) and salvianolic acids (SAs)—were selected as model drugs. In vitro Caco-2 cells transport and in vivo rat pharmacokinetics studies were conducted to examine the permeation effect of SNAC on R1 and SAs. R1, rosmarinic acid (RA), salvianolic acid B (SA-B) and salvianolic acid B (SA-A) were determined to compare the permeation enhancement of different drugs. The MTT assay results showed that SNAC had no toxicity to Caco-2 cells. The transepithelial electrical resistance (TEER) of Caco-2 cell monolayer displayed that SNAC facilitated passive transport of polar charged SAs through the membrane of epithelial enterocytes. The pharmacokinetics results demonstrated that area under the curve (AUC) of RA, SA-B and SA-A with administration of SAs containing SNAC was 35.27, 8.72 and 9.23 times than administration of SAs. Tmax of RA, SA-B and SA-A were also prolonged. The AUC of R1 with administration of R1 containing SNAC was 2.24-times than administration of R1. SNAC is more effective in promoting absorption of SAs than R1. The study demonstrated that SNAC significantly improved bioavailability of R1 and SAs. What’s more, the effect of SNAC on absorption enhancement of charged drugs was larger than that of non-charged drugs. The current findings not only confirm the usefulness of SNAC for the improved delivery of R1 and SAs but also demonstrate the importance of biopharmaceutics characterization in the dosage form development of drugs.

scholarly journals Rectal Absorption of Ozagrel from a Suppository Containing Its Commercial Tablet in Healthy Human Subjects.

1997 ◽  
Vol 20 (3) ◽  
pp. 282-284
Author(s):  
Nian Xin ZHENG ◽  
Hitoshi SATO ◽  
Fumiaki KOBAYASHI ◽  
Yoh MASUKO ◽  
Isao ADACHI ◽  
...  
Keyword(s):  
Human Subjects ◽  
Rectal Absorption ◽  
Healthy Human ◽  
Healthy Human Subjects

Rectal absorption enhancement of peptide drugs

1990 ◽  
Vol 13 (2-3) ◽  
pp. 241-246 ◽  
Author(s):  
A.G. De Boer ◽  
E.J. van Hoogdalem ◽  
C.D. Heijligers-Feijen ◽  
J. Verhoef ◽  
D.D. Breimer
Keyword(s):  
Absorption Enhancement ◽  
Peptide Drugs ◽  
Rectal Absorption

Enhancement of Rectal Absorption of Rifampicin by Sodium para-Aminosalicylate Dihydrate in Human Subjects

1994 ◽  
Vol 114 (11) ◽  
pp. 894-900 ◽  
Author(s):  
Ryota SUZUKI ◽  
Yuko NAKAJIMA ◽  
Naomi YAGI ◽  
Harumi KENMOTSU ◽  
Hitoshi SEKIKAWA ◽  
...  
Keyword(s):  
Human Subjects ◽  
Rectal Absorption

scholarly journals Nasal Delivery of Recombinant Human Growth Hormone: In Vivo Evaluation with Pheroid™ Technology and N-Trimethyl Chitosan Chloride

2010 ◽  
Vol 13 (2) ◽  
pp. 263 ◽  
Author(s):  
Dewald Steyn ◽  
Lissinda Hester Du Plessis ◽  
Awie Kotze
Keyword(s):  
Growth Hormone ◽  
Human Growth Hormone ◽  
Recombinant Human Growth Hormone ◽  
Subcutaneous Administration ◽  
Human Growth ◽  
Absorption Enhancement ◽  
Control Group ◽  
Absorption Enhancers ◽  
Trimethyl Chitosan

Purpose. It was the aim of this study to investigate the possible enhancement of the absorption of recombinant human growth hormone (rhGH) in the nasal cavity, in the presence of a polymeric absorption enhancer, N-trimethyl chitosan chloride (TMC) and a fatty acid-based delivery system, Pheroid™. Methods. Two types of Pheroid™ formulations, Pheroid™ vesicles and Pheroid™ microsponges were characterized and evaluated with regard to particle size and morphology. In vivo bioavailability studies in rats were performed and the nasal bioavailability of Pheroid™ vesicles and Pheroid ™microsponges were compared relative to subcutaneous administration. The results were also compared with different N-trimethyl chitosan chloride (TMC) formulations, TMC H-L and TMC H-H, well studied absorption enhancers. Results. Pheroid™ vesicles and Pheroid™ microsponges showed a size distribution of approxiamately 2-3 µm and 3-4 µm for Pheroid™ vesicles and Pheroid™ microsponges respectively. Using specific RIA, the relative bioavailability of rhGH after comparison with subcutaneous injection was determined to be 38.9, 128.5, 39.9, 136.3, and 8.3 % for Pheroid™ microsponges, Pheroid™ vesicles, TMC H-H, TMC H-L and control group (intranasal rhGH alone), respectively. All the enhancers showed significant absorption enhancement (P < 0.05) with the highest effect observed with TMC H-L. Conclusion. All the enhancers may have promising potential as safe and effective nasal absorption enhancers of rhGH.

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